Assay Detail
Binding
CHEMBL2390167
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ORAl1/2/3 in HEK293 cells assessed as inhibition of Cd2+ influx after 10 mins by FLIPR assay in presence of thapsigargin
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Design, synthesis and pharmacological characterization of analogs of 2-aminoethyl diphenylborinate (2-APB), a known store-operated calcium channel blocker, for inhibition of TRPV6-mediated calcium transport.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.02 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386000 | — | — | 1 | 5.66 |
| CHEMBL2386180 | — | — | 1 | 5.62 |
| CHEMBL2386179 | — | — | 1 | 5.57 |
| CHEMBL2386172 | — | — | 1 | 5.50 |
| CHEMBL2386185 | — | — | 1 | 5.31 |
| CHEMBL2385996 | — | — | 1 | 5.29 |
| CHEMBL2386174 | — | — | 1 | 5.23 |
| CHEMBL2386184 | — | — | 1 | 5.19 |
| CHEMBL2386186 | — | — | 1 | 5.14 |
| CHEMBL2386009 | — | — | 1 | 5.13 |
| CHEMBL2386181 | — | — | 1 | 5.11 |
| CHEMBL2385999 | — | — | 1 | 5.09 |
| CHEMBL81556 | DIPHENYL BORINIC ACID | — | 1 | 5.06 |
| CHEMBL2386171 | — | — | 1 | 5.02 |
| CHEMBL2386004 | — | — | 1 | 5.01 |
| CHEMBL2386177 | — | — | 1 | 5.01 |
| CHEMBL2386178 | — | — | 1 | 5.00 |
| CHEMBL2385998 | — | — | 1 | 5.00 |
| CHEMBL2386001 | — | — | 1 | 4.99 |
| CHEMBL2385997 | — | — | 1 | 4.99 |
| CHEMBL2386011 | — | — | 1 | 4.98 |
| CHEMBL2386003 | — | — | 1 | 4.96 |
| CHEMBL2386010 | — | — | 1 | 4.93 |
| CHEMBL2385995 | — | — | 1 | 4.92 |
| CHEMBL2386188 | — | — | 1 | 4.87 |
| CHEMBL2386005 | — | — | 1 | 4.83 |
| CHEMBL2386173 | — | — | 1 | 4.77 |
| CHEMBL2386183 | — | — | 1 | 4.60 |
| CHEMBL2386008 | — | — | 1 | 4.59 |
| CHEMBL2386175 | — | — | 1 | 4.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386000 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2386180 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2386179 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2386172 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2386185 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL2385996 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL2386174 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2386184 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL2386186 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL2386009 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL2386181 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL2385999 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL81556 | DIPHENYL BORINIC ACID | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL2386171 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL2386177 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL2386004 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL2386178 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL2385998 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL2386001 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL2385997 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL2386011 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL2386003 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2386010 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL2385995 | — | IC50 | = | 11900.0 | nM | 4.92 |
| CHEMBL2386188 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL2386005 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL2386173 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL2386183 | — | IC50 | = | 25200.0 | nM | 4.60 |
| CHEMBL2386008 | — | IC50 | = | 25900.0 | nM | 4.59 |
| CHEMBL2386175 | — | IC50 | = | 25800.0 | nM | 4.59 |
| CHEMBL2386176 | — | IC50 | = | 36400.0 | nM | 4.44 |
| CHEMBL2386006 | — | IC50 | = | 44600.0 | nM | 4.35 |
| CHEMBL2386007 | — | IC50 | = | 184200.0 | nM | - |
| CHEMBL257679 | METHANE BORONIC ACID | IC50 | > | 500000.0 | nM | - |
| CHEMBL2386190 | DIPHENYLMETHANOL | IC50 | > | 500000.0 | nM | - |
| CHEMBL657 | DIPHENHYDRAMINE | IC50 | > | 500000.0 | nM | - |